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Assay Detail

CHEMBL2076249

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
TP_TRANSPORTER: drug resistance (vincristine) in AML-2/D100 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type AML-2/D100
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

ATP-dependent translocase ABCB1 (CHEMBL4302)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Reversal of P-glycoprotein-mediated MDR by 5,7,3',4',5'-pentamethoxyflavone and SAR.
Choi CH, Kim JH, Kim SH.
Biochem Biophys Res Commun (2004) 320 : 672 -679
PubMed 15240100 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.62 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6966 VERAPAMIL 4.0 1 6.40
CHEMBL2074901 1 6.40
CHEMBL370963 1 6.05
CHEMBL91153 3',4'-DIMETHOXYFLAVONE 1 5.92
CHEMBL13473 7,3',4'-Trimethoxyflavone 1 5.92
CHEMBL1087720 TRIMETHYLAPIGENIN 1 5.85
CHEMBL2074919 1 5.72
CHEMBL75258 1 5.50
CHEMBL226507 SINENSETIN 1 5.50
CHEMBL575072 1 5.20
CHEMBL151 LUTEOLIN 2.0 1 4.71
CHEMBL50 QUERCETIN 3.0 1 4.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6966 VERAPAMIL IC50 = 400.0 nM 6.40
CHEMBL2074901 IC50 = 400.0 nM 6.40
CHEMBL370963 IC50 = 900.0 nM 6.05
CHEMBL91153 3',4'-DIMETHOXYFLAVONE IC50 = 1200.0 nM 5.92
CHEMBL13473 7,3',4'-Trimethoxyflavone IC50 = 1200.0 nM 5.92
CHEMBL1087720 TRIMETHYLAPIGENIN IC50 = 1400.0 nM 5.85
CHEMBL2074919 IC50 = 1900.0 nM 5.72
CHEMBL75258 IC50 = 3200.0 nM 5.50
CHEMBL226507 SINENSETIN IC50 = 3200.0 nM 5.50
CHEMBL575072 IC50 = 6300.0 nM 5.20
CHEMBL151 LUTEOLIN IC50 = 19600.0 nM 4.71
CHEMBL50 QUERCETIN IC50 = 52500.0 nM 4.28